The ring of benzene is among the most popular structural elements in chemistry. Every chemist from all disciplines - inorganic, polymer, physical, medicinal and organic chemistry - deals with derivatives of benzene. For example, it is one of the most popular rings in natural products and the most popular ring in bioactive compounds. Moreover, more than five hundred drugs and agrochemicals, including the well-known Aspirin and Paracetamol are benzene-containing molecules.
On the other hand, during the recent years pharmaceutical companies struggle to deliver novel drugs to the market - ca. 96% of all modern medicinal projects fail. In part, it happens because of a lack of innovative, practical approaches leading to novel “drug-like” organic molecules. Medicinal chemists still mostly use the old benzene-containing building blocks discovered the last century - substituted anilines, benzoic acids, phenols, etc.
In this context, at the moment pharmaceutical companies urgently need innovative practical methods and reagents to access the novel “chemical space.” And we - academic scientists - must address this issue to help pharmaceutical companies to decrease the attrition rate.
In this project, we want to (a) develop for the first time the saturated bioisosteres for ortho- and meta-substituted benzenes; (b) study their physichochemical characteristics (solubility, lipophilicity, metabolic stability); (c) incorporate the most promising cores into benzene-containing drugs and agrochemicals (Aceclofenac, Ketoprofen, Boscalid), and to study their biological activity and physico-chemical properties.
